{"product_id":"varenicline-bhb21900008","title":"Varenicline","description":"\u003cdiv class=\"bhp-desc\"\u003e\n\u003cstyle\u003e.bhp-desc{font-size:16px;color:#1a1a1a;line-height:1.7}.bhp-desc h2{font-size:18px;font-weight:700;color:#003366;margin:24px 0 10px;padding-bottom:6px;border-bottom:2px solid #003366}.bhp-desc p{margin:0 0 12px}.bhp-desc .bhp-spec-table{width:100%;border-collapse:collapse;margin:12px 0 18px}.bhp-desc .bhp-spec-table th{width:36%;text-align:left;padding:8px 12px;background:#e8f0fb;color:#003366;font-weight:600;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-spec-table td{padding:8px 12px;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-warning-box{background:#fff8e6;border-left:4px solid #e6a817;padding:10px 14px;margin:10px 0 14px;border-radius:0 4px 4px 0}.bhp-desc .bhp-cat-pill{display:inline-block;background:#003366;color:#fff;border-radius:20px;padding:3px 12px;font-size:13px;margin-bottom:10px}\u003c\/style\u003e\n\u003cspan class=\"bhp-cat-pill\"\u003eAgonists\u003c\/span\u003e\u003ch2\u003eCompound Overview\u003c\/h2\u003e\n\u003cp\u003eVarenicline, also known as CP 526555, is an orally active partial agonist at the α4β2 nicotinic acetylcholine receptor (α4β2 nAChR), the principal mediator of nicotine dependence, with an IC\u003csub\u003e50\u003c\/sub\u003e of 250 nM. The compound also acts as a partial agonist at α6β2 nAChR and a full agonist at α7β2 nAChR. It blocks the direct agonist effects of nicotine on nAChR while itself stimulating nAChR in a more moderate way, and it has been widely used as an aid to smoking cessation\u003csup\u003e[1][2][3][4][5]\u003c\/sup\u003e. It is supplied as a light yellow to yellow solid (C13H13N3, MW 211.27) at 99.92% purity.\u003c\/p\u003e\n\u003ch2\u003ePhysical \u0026amp; Chemical Properties\u003c\/h2\u003e\n\u003ctable class=\"bhp-spec-table\"\u003e\u003ctbody\u003e\n\u003ctr\u003e\n\u003cth\u003eCAS Number\u003c\/th\u003e\n\u003ctd\u003e249296-44-4\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC13H13N3\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e211.27 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e99.92%\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eAppearance\u003c\/th\u003e\n\u003ctd\u003eSolid\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eColor\u003c\/th\u003e\n\u003ctd\u003eLight yellow to yellow\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSMILES\u003c\/th\u003e\n\u003ctd\u003eC12=C(C=C3N=CC=NC3=C2)C4CC1CNC4\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003eMembrane Transporter\/Ion Channel; Neuronal Signaling\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSolubility\u003c\/th\u003e\n\u003ctd\u003eIn Vitro: H2O: ≥ 20 mg\/mL (94.67 mM)\u003cbr\u003eDMSO: 20 mg\/mL (94.67 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * \"≥\" means soluble, but saturation unknown.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eStorage\u003c\/th\u003e\n\u003ctd\u003ePowder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eShipping\u003c\/th\u003e\n\u003ctd\u003eRoom temperature in continental US; may vary elsewhere.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eBiological Activity\u003c\/h2\u003e\n\u003ch3 style=\"font-size:16px;font-weight:700;color:#003366;margin:16px 0 8px\"\u003eActivity \u0026amp; Target\u003c\/h3\u003e\n\u003cp\u003eEC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)\u003csup\u003e[1]\u003c\/sup\u003e\u003c\/p\u003e\n\u003ch2\u003eLiterature Cited\u003c\/h2\u003e\n\u003cp style=\"font-size:14px;color:#555;margin:0 0 10px\"\u003e\u003cem\u003eSources cited in this description and in the In Vitro \u0026amp; In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.\u003c\/em\u003e\u003c\/p\u003e\n\u003cp\u003e [1]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/25005652\/\"\u003eKoegelenberg CF, et al. Efficacy of varenicline combined with nicotine replacement therapy vs varenicline alone for smoking cessation: a randomized clinical trial. JAMA. 2014 Jul;312(2):155-61.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [2]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/30872534\/\"\u003eMagnus CJ, et al. Ultrapotent chemogenetics for research and potential clinical applications. Science. 2019;364(6436):eaav5282.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [3]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/28842382\/\"\u003eKoga M, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017;390:1-9.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [4]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/32294065\/\"\u003eRen J, et al. Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594. Anesthesiology. 2020 May;132(5):1197-1211.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [5]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/24304823\/\"\u003eMello NK, et al. Effects of chronic varenicline treatment on nicotine, cocaine, and concurrent nicotine+cocaine self-administration. Neuropsychopharmacology. 2014 Apr;39(5):1222-31.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [6]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/19168054\/\"\u003eRollema H, et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect. Eur J Pharmacol. 2009 Mar 1;605(1-3):114-6.\u003c\/a\u003e\u003c\/p\u003e\n\u003ch2\u003eSafety\u003c\/h2\u003e\n\u003cdiv class=\"bhp-warning-box\"\u003e\u003cp\u003e\u003cstrong\u003eFor Research Use Only.\u003c\/strong\u003e Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.\u003c\/p\u003e\u003c\/div\u003e\n\u003c\/div\u003e","brand":"MedChemExpress (MCE)","offers":[{"title":"5 mg","offer_id":67604847952237,"sku":"HY-10019-5MG","price":72.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67604997996909,"sku":"HY-10019-10MG","price":108.0,"currency_code":"USD","in_stock":true},{"title":"25 mg","offer_id":67604998029677,"sku":"HY-10019-25MG","price":216.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67604998062445,"sku":"HY-10019-50MG","price":324.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67604998095213,"sku":"HY-10019-100MG","price":504.0,"currency_code":"USD","in_stock":true},{"title":"200 mg","offer_id":67604998127981,"sku":"HY-10019-200MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"500 mg","offer_id":67604998160749,"sku":"HY-10019-500MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"1 mL x 10 mM (in DMSO)","offer_id":67604998193517,"sku":"HY-10019-1MLX10MM","price":80.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-10019.gif?v=1790972871","url":"https:\/\/www.ebiohippo.com\/products\/varenicline-bhb21900008","provider":"BioHippo","version":"1.0","type":"link"}